145011-61-6Relevant articles and documents
Process and intermediates for bis-aza-bicyclic anxiolytic agents
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, (2008/06/13)
Optically pure intermediates of formula (1) wherein the substituent B is either cis or trans to the C9a -C1 bond and is selected from the group consisting of --CH2 OH, --CHO, --CH2 OSO2 R, --CH2 CN, --CH(OH)CH2 NO2, --CH=CH--NO2, (2) and (3), C is selected from the group consisting of --H, (4), (5), and a nitrogen protecting group which is removable by hydrogenation or acid treatment; and wherein R is (C1 -C8) alkyl, phenyl or alkyl substituted phenyl; X is N or CH; Y is O or S and Z is H or Cl; for the synthesis of octahydro-1H-pyrido(1,2-a)pyrazinyl ethyl carboxamide anxiolytic agents.
Process and intermediate for certain bis-aza-bicyclic anxiolytic agents
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, (2008/06/13)
(C1 -C3)Alkyl-4,6,7,8,9,9a-hexahydro-2H,3H-pyrido[1,2-a]pyrazin-1-one-7-carboxylate esters, important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C1 -C3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates, di(C1 -C3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicarboxylates. In the process, the starting material is reacted with either 2-(phthalimido)ethyl triflate or 2-(phthalimido)acetaldehyde to form the new intermediate, which can then be cyclized to the aforementioned precursor.
Process and intermediate for certain bis-aza-bicyclic anxiolytic agents
-
, (2008/06/13)
(C1 -C3)Alkyl-4,6,7,8,9,9a-hexahydro-2H,3H-pyrido-[1,2-a]pyrazin-1-one-7-carboxylate esters, important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C1 -C3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates, di(C1 -C3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicarboxylates. In the process, the starting material is reacted with either 2-(phthalimido)ethyl triflate or 2-(phthalimido)acetaldehyde to form the new intermediate, which can then be cyclized to the aforementioned precursor.